1. Field of the Invention
The invention relates to pharmaceutically active dibenzoazepine-based tetracyclics, or more specifically, dibenzoazepine-based tetracyclics having anxiolytic properties.
2. Description of the Prior art, and Other Information
Compounds according to general formula I in which the --OR moiety is missing are known, inter alia from U.S. Pat. No. 3,534,041 (which reveals the compound now known as "GB-94"-see below) and its progeny, U.S. Pat. No. 4,025,513 and copending application United States Ser. No. 754,216 (not prior art to the instant invention), Canadian Pat. Nos. 965,091, 895,301, all incorporated herein, and application Ser. No. 219,742 (not prior art to the instant invention). See Also U.S. Pat. No. 4,128,641 to Itil (not prior art to the instant invention--issued Dec. 5, 1978), which discloses another use of GB-94, i.e., ##STR2## as a neuroleptic agent for schizophrenic patients.
In addition to pronounced antihistamine and anti-serotonin activities, the pharmacological profile of these known compounds includes potent anti-depressive and sedative properties.
Also of interest are (1) U.S. Pat. No. 3,701,778 (Van der Burg), which discloses tetracyclics having any of sulfur, oxygen, or N(C.sub.1 -C.sub.6) in the 10-position; (2) U.S. Pat. No. 3,917,633 (alkyl substitutes, aminoalkyl, or alkyl aminoalkyl substituents; (3) U.S. Pat. No. 3,959,470, disclosing 3-methyl-8-methoxy- 3H,1,2,5,6-tetrahydropyrazino-[1,2,3]-ab-.beta.-carbolin (anti-depressants); (4) U.S. Pat. No. 3,966,723, teaching a dibenzoazepine-based tetracyclic ring system wherein the 10-position can have a methyl or dimethyl substituent (anti-depressants); (5) U.S. Pat. No. 4,062,848; and (6) British Pat. No. 1,468,632 (no 10-substitution).